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Compound class:
Peptide or derivative
Comment: This peptide is a RXFP3/RXFP4 antagonist [2]. It behaves as a RXFP4 partial agonist (of cAMP activation) in CHO cells expressing human RXFP4. Structurally it is a chimeric peptide made of the A-chain of INSL5 and a C-terminally truncated B-chain of H3 relaxin [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Kuei C, Sutton S, Bonaventure P, Pudiak C, Shelton J, Zhu J, Nepomuceno D, Wu J, Chen J, Kamme F et al.. (2007)
R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization. J Biol Chem, 282 (35): 25425-35. [PMID:17606621] |
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2. Praveen P, Bathgate RAD, Hossain MA. (2019)
Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4. Sci Rep, 9 (1): 17828. [PMID:31780677] |
